A patent review of berberine and its derivatives with various pharmacological activities (2016–2020)

ABSTRACT

Introduction

Berberine (BBR), as one of the outstanding representatives of isoquinoline alkaloids, has been used as an antibacterial drug for a long time in China since ancient times. Currently, a large number of studies have been reported that berberine has a wide spectrum of pharmacological activities, such as anti-tumor, anti-inflammatory, hypoglycemic, hypolipidemic, anti-obesity, and the like.

Areas covered

This review systematically discussed important patents on berberine and berberine derivatives in terms of pharmacological activity between 2016 and 2020. These patents were mainly searched through the European Patent Office database and Web of Science. These berberine patents (~41) cover a wide range of applications, mainly including antitumor, anti-inflammatory, antibacterial, anti-metabolic disorder, and other newly reported pharmacological activities.

Expert opinion

Berberine is an important lead compound with great potential for optimization in drug development. However, there is a lack of research related to the biomolecular targets of BBR, which directly restricts the development of berberine in the pharmaceutical field. The problems involved with poor bioavailability and cytotoxicity are also worth considering in the development of berberine-based drugs. Accordingly, the increasing number of patents involving biomolecular targets in BBR’s patent applications will be published as its related pharmacological mechanisms are further deciphered.

KEYWORDS:

• Berberine
• antitumor
• anti-inflammatory
• antibacterial
• anti-diabetic
• derivative

Article highlights

• A number of patents of berberine and its derivatives covering various therapeutic effects in a wide range of time from 2016 to 2020, is reviewed.

• A large of proportion of berberine-based patents in this review are correlated with the treatment of cancer and metabolic disorder.

• Except for the commonly therapeutic effects against cancer, inflammation, and cardiovascular diseases as reported previously, berberine would display several new pharmacological activities such as being anti-phenylketonuria, anti-depressed, and antiallergic.

Berberine and its derivatives would be preferentially applied for the treatment of cardiovascular disease and metabolic disorders.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This work was supported by the Project for Young Teachers of Nanjing Forestry University (grant number: CX2017005), a Project funded by the National First-class Disciplines (PNFD).